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    Activator of peroxisome proliferator-activated receptor delta
    1.
    发明申请
    Activator of peroxisome proliferator-activated receptor delta 有权
    过氧化物酶体增殖物激活受体δ的活化剂

    公开(公告)号：US20080009525A1

    公开(公告)日：2008-01-10

    申请号：US11888493

    申请日：2007-07-31

    申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    IPC分类号： A61K31/4439 ,  A61K31/422 ,  C07D263/02 ,  C07D403/00 ,  C07D417/00 ,  C07D413/00 ,  C07D277/04 ,  A61K31/427

    CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

    摘要： A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

    摘要翻译： 由以下通式（I）表示的化合物：（其中R 1表示苯基等，其可以具有选自C 1-8烷基的取代基 具有卤素，卤素，羟基等的C 1-8烷基; R 2表示C 1-8烷基等; A 表示氧，硫等; X表示C 1-8亚烷基链等; Y表示C（-O），CH-CH等; R 3 O R 4，R 5和R 5各自表示氢，C 1-8烷基等; B表示CH或氮; Z表示 氧或硫; R 6和R 7各自表示氢，C 1-8烷基等;和R 8， / SUP>表示氢或C 1-8烷基，条件是R 3，R 4和R 4中的至少一个， 5不是氢）或化合物的盐; 和含有该化合物或盐作为活性成分的PPAR-δ活化剂。

    PPAR delta activators
    4.
    发明授权
    PPAR delta activators 有权
    PPARδ激活剂

    公开(公告)号：US06787552B2

    公开(公告)日：2004-09-07

    申请号：US10344496

    申请日：2003-02-11

    申请人： Shogo Sakuma ,  Tsuyoshi Endo ,  Atsushi Tendo ,  Toshihiro Takahashi ,  Shinichi Yoshida ,  Kunio Kobayashi ,  Nobutaka Mochizuki ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    发明人： Shogo Sakuma ,  Tsuyoshi Endo ,  Atsushi Tendo ,  Toshihiro Takahashi ,  Shinichi Yoshida ,  Kunio Kobayashi ,  Nobutaka Mochizuki ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    IPC分类号： A61K31421

    CPC分类号： C07D413/04 ,  C07D263/32 ,  C07D277/24

    摘要： Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.

    摘要翻译： 通式（I）的化合物或其盐和含有化合物或其盐作为活性成分的PPARdta（过氧化物酶体增殖物活化受体δ）的活化剂：其中R 1和R 2各自为氢，C 1-8 烷基，可被取代的芳基或杂环基等; A是氧，硫等; X 1和X 2各自为自由价，氧，S（O）p（其中p为0至2的整数），C（= O），C（= O）NH，NHC（= O），CH = CH等; Y是任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基，条件是当X 1是自由价时，X 2不是O或S（O）p，而当X 1是C（O） = O）NH，X 2不是自由价。

    Quinoline derivatives
    5.
    发明授权
    Quinoline derivatives 失效
    喹啉衍生物

    公开(公告)号：US5693651A

    公开(公告)日：1997-12-02

    申请号：US809592

    申请日：1997-03-26

    申请人： Yutaka Nomura ,  Shogo Sakuma ,  Seiichiro Masui

    发明人： Yutaka Nomura ,  Shogo Sakuma ,  Seiichiro Masui

    IPC分类号： A61K31/4709 ,  A61P3/10 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  A61K31/47

    CPC分类号： C07D413/06 ,  C07D417/06 ,  C07D417/14

    摘要： The invention has an object to provide a novel quinoline derivative of the following formula (I) which has no benzyl group in the 5-position and shows hypoglycemic effect, particularly, by oral administration: ##STR1## in which R.sup.1 is hydrogen; an alkyl group of 1-6 carbon atoms, an amino group of the formula of --NR.sup.4 R.sup.5 in which each of R.sup.4 and R.sup.5 independently is hydrogen, alkyl of 1-6 carbon atoms, phenyl, pyridyl, pyrimidyl or benzoyl; or a phenyl group, a naphthyl group, a cycloalkyl group having 3 to 8 carbon atoms, or a 5 to 8 membered heterocyclic group comprising, as ring-constituting atoms, 1 to 2 nitrogens, oxygens or sulfurs and remaining carbon atoms, each of which may have, as a substituent, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, hydroxyl, halogenoalkyl of 1-6 carbon atoms, halogenoalkoxy of 1-6 carbon atoms, nitro, amino, phenyl, thienyl, furyl, thiazolyl or pyridyl; Z is O, S, C.dbd.O, or CH.sub.2 ; E is S or O; m is an integer of 0 to 4; p is an integer of 0 to 4; q is an integer of 0 to 4; and the double line composed of a broken line and a solid line means a single or double bond.

    摘要翻译： PCT No.PCT / JP95 / 02167 Sec。 371日期1997年3月26日 102（e）1997年3月26日PCT PCT 1995年10月20日PCT公布。 出版物WO96 / 日期：1996年5月2日本发明的目的是提供下述式（I）的喹啉衍生物，其在5-位没有苄基，具有低血糖作用，特别是通过口服给药：（I） 其中R1是氢; 1-6个碳原子的烷基，-NR4R5的氨基，其R4和R5各自独立地为氢，1-6个碳原子的烷基，苯基，吡啶基，嘧啶基或苯甲酰基; 或苯基，萘基，具有3-8个碳原子的环烷基或5至8元杂环基，其包含作为构成环的原子的1至2个氮，氧或硫和剩余的碳原子 其可以具有1-6个碳原子的烷基，1-6个碳原子的烷氧基，1-6个碳原子的卤素，羟基，卤代烷基，1-6个碳原子的卤代烷氧基，硝基，氨基，苯基， 噻吩基，呋喃基，噻唑基或吡啶基; Z是O，S，C = O或CH 2; E是S或O; m为0〜4的整数。 p为0〜4的整数。 q是0〜4的整数; 由虚线和实线构成的双线表示单键或双键。

    Activator of peroxisome proliferator-activated receptor δ
    6.
    发明授权
    Activator of peroxisome proliferator-activated receptor δ 有权
    过氧化物酶体增殖物激活受体δ的活化剂

    公开(公告)号：US07652045B2

    公开(公告)日：2010-01-26

    申请号：US11888493

    申请日：2007-07-31

    申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    IPC分类号： A61K31/421 ,  A61K31/426 ,  C07D263/30 ,  C07D277/20

    CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

    摘要： A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

    摘要翻译： 由以下通式（I）表示的化合物：（其中R 1表示可以具有选自C 1-8烷基，具有卤素的C 1-8烷基，卤素，羟基等的取代基的苯基等; R 2 表示C1-8烷基等; A表示氧，硫等; X表示C1-8亚烷基链等; Y表示C（-O），CH-CH等; R3，R4和R5 各自表示氢，C 1-8烷基等; B表示CH或氮; Z表示氧或硫; R6和R7各自表示氢，C1-8烷基等; R8表示氢或C1-8烷基; R3，R4和R5中的至少一个不是氢）或化合物的盐; 和含有该化合物或盐作为活性成分的PPAR-δ活化剂。

    Activator for peroxisome proliferator-activated receptor δ
    7.
    发明授权
    Activator for peroxisome proliferator-activated receptor δ 有权
    过氧化物酶体增殖物激活受体δ的活化剂

    公开(公告)号：US07648999B2

    公开(公告)日：2010-01-19

    申请号：US11888492

    申请日：2007-07-31

    申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    IPC分类号： A61K31/426 ,  A61K31/4436 ,  A61K31/4709 ,  C07D277/22 ,  C07D417/04

    CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

    摘要： A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

    摘要翻译： 由以下通式（I）表示的化合物：（其中R 1表示可以具有选自C 1-8烷基，具有卤素的C 1-8烷基，卤素，羟基等的取代基的苯基等; R 2 表示C1-8烷基等; A表示氧，硫等; X表示C1-8亚烷基链等; Y表示C（-O），CH-CH等; R3，R4和R5 各自表示氢，C 1-8烷基等; B表示CH或氮; Z表示氧或硫; R6和R7各自表示氢，C1-8烷基等; R8表示氢或C1-8烷基; R3，R4和R5中的至少一个不是氢）或化合物的盐; 和含有该化合物或盐作为活性成分的PPAR-δ活化剂。

    Activator of peroxisome proliferator-activated re-ceptor δ
    10.
    发明授权
    Activator of peroxisome proliferator-activated re-ceptor δ 有权
    过氧化物酶体增殖物激活的受体δ激动剂

    公开(公告)号：US07265137B2

    公开(公告)日：2007-09-04

    申请号：US10486783

    申请日：2002-08-02

    申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

    IPC分类号： A61K31/421 ,  A61K31/426 ,  C07D213/30 ,  C07D277/20

    CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

    摘要： A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

    摘要翻译： 由以下通式（I）表示的化合物：（其中R 1表示苯基等，其可以具有选自C 1-8烷基的取代基 具有卤素，卤素，羟基等的C 1-8烷基; R 2表示C 1-8烷基等; A 表示氧，硫等; X表示C 1-8亚烷基链等; Y表示C（-O），CH-CH等; R 3 O R 4，R 5和R 5各自表示氢，C 1-8烷基等; B表示CH或氮; Z表示 氧或硫; R 6和R 7各自表示氢，C 1-8烷基等;和R 8， / SUP>表示氢或C 1-8烷基，条件是R 3，R 4和R 4中的至少一个， 5不是氢）或化合物的盐; 和含有该化合物或盐作为活性成分的PPAR-δ活化剂。